Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.
Bioorg Med Chem Lett. 2010 Oct 15;20(20):6116-20. doi: 10.1016/j.bmcl.2010.08.037. Epub 2010 Aug 18.
Novel bottromycin derivatives were synthesized from bottromycin A(2) via a hydrazide derivative as a common intermediate. Seventeen derivatives were subjected to in vitro evaluation against drug-resistant gram-positive bacteria. Some compounds showed potent anti-MRSA and anti-VRE activity, as did bottromycin A(2). Notably, a propyl ketone derivative exhibited good antibacterial activity with excellent metabolite stability.
新型博替霉素衍生物是通过博替霉素 A（2）的酰肼衍生物作为共同的中间体合成的。对 17 种衍生物进行了抗耐药性革兰氏阳性菌的体外评估。一些化合物表现出对 MRSA 和 VRE 的有效抑制活性，与博替霉素 A（2）相似。值得注意的是，一种丙基酮衍生物具有良好的抗菌活性和出色的代谢物稳定性。
